- Neutrophil Elastase Promotes Linker Cleavage and Paclitaxel Release from an Integrin-Targeted Conjugate
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This work takes advantage of one of the hallmarks of cancer, that is, the presence of tumor infiltrating cells of the immune system and leukocyte-secreted enzymes, to promote the activation of an anticancer drug at the tumor site. The peptidomimetic integrin ligand cyclo(DKP-RGD) was found to accumulate on the surface of αvβ3 integrin-expressing human renal cell carcinoma 786-O cells. The ligand was conjugated to the anticancer drug paclitaxel through a Asn-Pro-Val (NPV) tripeptide linker, which is a substrate of neutrophil-secreted elastase. In vitro linker cleavage assays and cell antiproliferative experiments demonstrate the efficacy of this tumor-targeting conjugate, opening the way to potential therapeutic applications.
- Raposo Moreira Dias, André,Pina, Arianna,Dean, Amelia,Lerchen, Hans-Georg,Caruso, Michele,Gasparri, Fabio,Fraietta, Ivan,Troiani, Sonia,Arosio, Daniela,Belvisi, Laura,Pignataro, Luca,Dal Corso, Alberto,Gennari, Cesare
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Read Online
- Camptothecin derivatives and their medical use
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The invention aims at providing camptothecin derivatives represented by a formula I as shown in the specification and pharmaceutically acceptable non-toxic salts, hydrates or solvates thereof. In the formula I, R1 and R4 represent H or C1-C5 alkyls; R2 represents an alkyl side chain of an L-type or D-type amino acid, namely H, -CH3, -CH(CH3)2, -CH2CH(CH3)2 or -CH(CH3)CH2CH3; R3 represents H or -CH2N(CH3)2; n is 0 or an integer ranging from 1 to 6.
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Paragraph 0083; 0085
(2018/07/07)
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- REAGENTS FOR QUANTITATIVE MASS SPECTROMETRY
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In some embodiments, a mass spectrometry tag may comprise a linker region, a mass balance region, and a reporter region. The mass spectrometry tag may be configured to fragment in a mass spectrometer via an energy dependent process to produce multiple reporter molecules. For example, the reporter region of the tag may be configured to produce at least two reporter molecules via fragmentation. In some embodiments, one or more regions of the tag may comprise at least one heavy isotope. In some such embodiments, the ability to fragment into multiple reporter molecules as well as the placement and/or number of heavy isotope(s) allows the mass spectrometry tag to be distinguished from other similar mass spectrometry tags. In some such embodiments, the ability to distinguish between tags having the same or substantially similar total mass to charge ratio and reporter region mass may allow the system to have a greater multiplexing capacity than conventional systems.
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Paragraph 0273; 0274
(2018/08/09)
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- A multicatalyst system for the one-pot desymmetrization/oxidation of meso-1,2-alkane diols
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Two is better than one: We demonstrate the viability of an organocatalytic reaction sequence along a short peptide backbone that carries two independent catalytic functionalities, which allow the rapid, one-pot acylative desymmetrization and oxidation of meso-alkane-1,2-diols to the corresponding acetylated acetoins with good yields and enantioselectivities (see scheme). Copyright
- Mueller, Christian E.,Hrdina, Radim,Wende, Raffael C.,Schreiner, Peter R.
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supporting information; experimental part
p. 6309 - 6314
(2011/08/07)
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- Synthesis of peptides and proteins
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Solid phase synthesis of peptides and proteins have been improved by the use of a trifunctional segment, one functional group of which is bound to a solid support, the other two functional groups being available as substrates upon which identical proteins are synthesized.
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